Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties. Many biological effects of melatonin are produced through activation of melatonin receptors, while others are due to its role as a pervasive and powerful antioxidant, with a particular role in the protection of nuclear and mitochondrial DNA.
Molecular Weight | 232.28 |
Formula | C13H16N2O2 |
CAS Number | 73-31-4 |
Solubility (25°C) | DMSO 80 mg/mL Ethanol 10 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Sankha Bhattacharya, et al. Melatonin and its ubiquitous anticancer effects
[2] Susanna Esposito, et al. Pediatric sleep disturbances and treatment with melatonin
[3] Fernanda Gaspar do Amaral, et al. A brief review about melatonin, a pineal hormone
[4] B Claustrat, et al. Melatonin: Physiological effects in humans
[5] Armando L Morera-Fumero, et al. Role of melatonin in schizophrenia
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S26131
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Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. |
4-P-PDOT
4-P-PDOT is a MT2-receptor-specific antagonist, it is >300-fold more selective for MT2 than MT1. |
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